Dupuy Jacques, Sutra Jean-François, Alvinerie Michel, Rinaldi Laura, Veneziano Vincenzo, Mezzino Laura, Pennacchio Saverio, Cringoli Giuseppe
INRA-UR66, Laboratoire de Pharmacologie-Toxicologie, B.P. 3, 31931 Toulouse Cedex 9, France.
Vet Parasitol. 2008 Nov 7;157(3-4):284-90. doi: 10.1016/j.vetpar.2008.07.027. Epub 2008 Aug 5.
The pharmacokinetics and mammary excretion of moxidectin and eprinomectin were determined in water buffaloes (Bubalus bubalis) following topical administration of 0.5mgkg(-1). Following administration of moxidectin, plasma and milk concentrations of moxidectin increased to reach maximal concentrations (C(max)) of 5.46+/-3.50 and 23.76+/-16.63ngml(-1) at T(max) of 1.20+/-0.33 and 1.87+/-0.77 days in plasma and milk, respectively. The mean residence time (MRT) were similar for plasma and milk (5.27+/-0.45 and 5.87+/-0.80 days, respectively). The AUC value was 5-fold higher in milk (109.68+/-65.01ngdayml(-1)) than in plasma (23.66+/-12.26ngdayml(-1)). The ratio of AUC milk/plasma for moxidectin was 5.04+/-2.13. The moxidectin systemic availability (expressed as plasma AUC values) obtained in buffaloes was in the same range than those reported in cattle. The faster absorption and elimination processes of moxidectin were probably due to a lower storage in fat associated with the fact that animals were in lactation. Nevertheless, due to its high excretion in milk and its high detected maximum concentration in milk which is equivalent or higher to the Maximal Residue Level value (MRL) (40ngml(-1)), its use should be prohibited in lactating buffaloes. Concerning eprinomectin, the C(max) were of 2.74+/-0.89 and 3.40+/-1.68ngml(-1) at T(max) of 1.44+/-0.20 and 1.33+/-0.0.41 days in plasma and milk, respectively. The MRT and the AUC were similar for plasma (3.17+/-0.41 days and 11.43+/-4.01ngdayml(-1)) and milk (2.70+/-0.44 days and 8.49+/-3.33ngdayml(-1)). The ratio of AUC milk/plasma for eprinomectin was 0.76+/-0.16. The AUC value is 20 times lower than that reported in dairy cattle. The very low extent of mammary excretion and the milk levels reported lower than the MRL (20ngml(-1)) supports the permitted use of eprinomectin in lactating water buffaloes.
在局部给予0.5mg/kg的莫西菌素和埃普利诺菌素后,测定了它们在水牛(Bubalus bubalis)体内的药代动力学和乳腺排泄情况。给予莫西菌素后,血浆和牛奶中莫西菌素的浓度升高,分别在1.20±0.33天和1.87±0.77天达到血浆和牛奶中的最大浓度(C(max)),分别为5.46±3.50和23.76±16.63ng/ml。血浆和牛奶的平均驻留时间(MRT)相似(分别为5.27±0.45天和5.87±0.80天)。牛奶中的AUC值(109.68±65.01ng·day/ml)比血浆中的高5倍(23.66±12.26ng·day/ml)。莫西菌素的AUC牛奶/血浆比值为5.04±2.13。在水牛中获得的莫西菌素全身可用性(以血浆AUC值表示)与在牛中报道的处于同一范围。莫西菌素更快的吸收和消除过程可能是由于与动物处于哺乳期相关的脂肪中储存较低。然而,由于其在牛奶中的高排泄以及在牛奶中检测到的高最大浓度,该浓度等于或高于最大残留限量值(MRL)(40ng/ml),因此在泌乳水牛中应禁止使用。关于埃普利诺菌素,血浆和牛奶中的C(max)分别在1.44±0.20天和1.33±0.41天为2.74±0.89和3.40±1.68ng/ml。血浆(3.17±0.41天和11.43±4.01ng·day/ml)和牛奶(2.70±0.44天和8.49±3.33ng·day/ml)的MRT和AUC相似。埃普利诺菌素的AUC牛奶/血浆比值为0.76±0.16。AUC值比奶牛中报道的低20倍。乳腺排泄程度非常低且牛奶水平低于MRL(20ng/ml),这支持了埃普利诺菌素在泌乳水牛中的允许使用。